Novel Antitubercular Agent-Loaded Liposomal Vesicles: Optimization, Characterization, and Cytotoxicity Studies-Reference-Cited by-同舟云学术

Novel Antitubercular Agent-Loaded Liposomal Vesicles: Optimization, Characterization, and Cytotoxicity Studies

Published:2023-04-11 Issue: Volume: Page:
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Author:

Obiedallah Manar M.¹,Mironov Maxim A.¹,Belyaev Danila V.²,Ene Antoaneta³,Vakhrusheva Diana V.⁴,Krasnoborova Svetlana Yu.⁴,Bershitsky Sergey Y.⁵,Shchepkin Daniil V.⁶,Minin Artem S.⁷,Ishmetova Rashida I.²,Ignatenko Nina K.²,Tolshchina Svetlana G.²,Fedorova Olga V.¹,Rusinov Gennady L.¹

Affiliation:

1. Ural Federal University

2. I. Postovsky Institute of Organic Synthesis, Ural Branch of the Russian Academy of Sciences

3. Dunarea de Jos University of Galati

4. National Medical Research Center of Phthisiopulmonology and Infectious Diseases, 22 Parts’ezda St., 50

5. Institute of Immunology and Physiology, Ural Branch of Russian Academy of Sciences

6. Institute of Natural Sciences and Mathematics, Ural Federal University

7. M.N. Mikheev Institute of Metal Physics of the Ural Branch of the Russian Academy of Sciences

Abstract

Abstract The treatment of tuberculosis is still a challenging process due to the wide spread of pathogen strains resistant to antibacterial drugs, as well as the undesirable effects of anti-tuberculosis therapy. Hence, the development of safe and effective new anti-antitubercular agents in addition to suitable nanocarrier systems has become of utmost importance and necessity. Our research aims to develop liposomal vesicles that contain newly synthesized compounds with antimycobacterial action. The compound being studied is a derivative of imidazo-tetrazine named 3- (3,5-dimethylpyrazole-1-yl) -6-(isopropylthio) imidazo [1,2-b] [1, 2, 4, 5] tetrazine (compound 1). Several factors that affect the liposomal characteristics were studied. The maximum encapsulation efficiency was 53.62 ± 0.09. The selected liposomal formulation T8* possessed mean particle size about 205.3 ± 3.94 nm with PDI 0.282, and zeta potential was + 36.37 ± 0.49 mv. The results of the in vitro release study indicated that the solubility of compound 1 was increased by its incorporation in liposomes. The free compound and liposomal preparation showed antimycobacterial activity against M. tuberculosis H37Rv (ATCC 27294) at MIC value 0.94–1.88 µg/ml. We are predicting that the liposomes may be a good candidate for delivering of new antitubercular drugs.

Publisher

Research Square Platform LLC

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